期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 3, 页码 610-613出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.12.032
关键词
9-Aminoacridine; Antimalarials; Blood-stage; Cinnamic acid; Liver-stage; Multi-target drugs; Plasmodium falciparum; Schizontocidal
资金
- FEDER through the POFC-COMPETE programme [FCOMP-01-0124-FEDER-020963]
- Portuguese national funds through Fundacao para a Ciencia e a Tecnologia [PTDC/QUI-QUI/116864/2010]
- Fundacao para a Ciencia e Tecnologia (FCT) [PTDC/SAU-MII/099118/2008, PEst-C/QUI/UI0081/2011, PEst-C/CTM/LA0011/2011]
- FCT [SFRH/BPD/62967/2009]
- Fundação para a Ciência e a Tecnologia [PTDC/QUI-QUI/116864/2010, PTDC/SAU-MII/099118/2008] Funding Source: FCT
Novel 9-aminoacridine derivatives were synthesized by linking the heteroaromatic core to different cinnamic acids through an aminobutyl chain. The test compounds demonstrated mid-nanomolar in vitro activity against erythrocytic stages of the chloroquine-resistant W2 strain of the human malaria parasite Plasmodium falciparum. Two of the most active derivatives also showed in vitro activity against liver-stage Plasmodium berghei, with activity greater than that of the reference liver-stage antimalarial primaquine. The compounds were not toxic to human hepatoma cells at concentrations up to 5 mu M. Hence, 9-(N-cinnamoylbutyl)aminoacridines are a new class of leads for prevention and treatment of malaria. (c) 2012 Elsevier Ltd. All rights reserved.
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